Synthesis and biological evaluation of a chitobiose-based peptide N-glycanase inhibitor library.
J Org Chem
; 74(2): 605-16, 2009 Jan 16.
Article
em En
| MEDLINE
| ID: mdl-19072094
ABSTRACT
Peptide N-glycanase (PNGase), the enzyme responsible for the deglycosylation of N-linked glycoproteins, has an active site related to that of cysteine proteases. Chitiobiose was equipped with electrophilic traps often used in cysteine protease inhibitors, and the resulting compounds were evaluated as PNGase inhibitors. We found that the electrophilic trap of the inhibitor has a great influence on the potency of the compounds with the chloromethyl ketone inhibitor being the first potent C-glycoside-based PNGase inhibitor.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Peptídeo-N4-(N-acetil-beta-glucosaminil) Asparagina Amidase
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Dissacarídeos
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Inibidores Enzimáticos
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Bibliotecas de Moléculas Pequenas
Limite:
Humans
Idioma:
En
Ano de publicação:
2009
Tipo de documento:
Article